Human Leukocyte Antigen (HLA)
-is a component of the MHC complex that presents antigens to the surface cell to induce an immune response.
MHC class I
-present peptides from proteins that break down inside the cell
-foreign antigens presented by MHC I attract cytotoxic T-cells
-bind to CD8+ receptors
MHC class II
-present antigens encountered outside of the cell
-stimulate the multiplication of T-helper cells
-bind to CD4+ receptors
true
HLA-induced hypersensitivities are not related to the concentration of the drug. T or F?
Hapten
-chemically reactive small molecule that binds to proteins or peptides
Hapten Hypothesis
-when haptens bind to drugs; this can form an immunogen that is presented to T-cells to illicit an immune response.
Stevens-Johnson Syndrome (SJS)
-severe skin rash characterized by mucosal lesions and blisters
-skin detachment affected <10% of BSA; Mortality <5%
Toxic Epidermal Necrolysis (TEN)
-severe skin rash characterized by major skin exfoliation
-skin detachment affecting >30% of BSA; Mortality >30%
carbamazepine/oxcarbazapine
When selecting alternatives to phenytoin, you should avoid ______
Allopurinol
-a xanthine oxidase inhibitor used to prevent formation of uric acid
-used in patients at risk for tumor lysis syndrome and gout
southeast asian
Which ethnicity is most hypersensitive to Allopurinol
prodrug
Clopidogrel is a _______
CYP2C19
Clopidogrel is metabolized by ________
intermediate metabolite
Prasugrel is first metabolized into a(n) _______ before it is active.
CYP3A4
Prasugrel & Ticagrelor are mainly metabolized by
equipotent
Ticagrelor & its metabolite are __________ as antiplatelet agents.
85%; 35%
________ of Ticagrelor remains unchanged; while ________ becomes orally bioavailable.
enhanced inhibition of platelet aggregation; increases bleeding risk
CYP2C19*17 gain of function allele will have what effect on clopidogrel and thus the body?
omeprazole & esomeprazole
___________ & ____________ can be prescribed with Clopidogrel to treat bleeding.
inactivates voltage gate-calcium channels to reduce neuronal excitability
Carbamazepine MOA?
induces its own metabolism
What is unique about carbamazepine?
Oxcarbazepine
What is the derivative of Carbamazepine?
CYP3A4
Carbamazepine is metabolized by _____
phenytoin and other aromatic anticonvulsants
Individuals who are HLA-B*15:02 should avoid _______
abacavir
Individuals who are HLA-B *57:01 should avoid _______
b
Which is true about Ticagrelor (Brilinta)
a. it is a prodrug
b. it escapes the first pass effect
c. it has PGx issues
d. it isn't metabolized by CYP3A4 at all
a, b
Which is true about Prasugrel (Effient)
a. it is a pro drug
b. metabolized by CYP3A4
c. has PGx issues
d. inactivated via sulfation
CYP2C19
Clopidogrel is metabolized by ________
increased bleeding
UM metabolizers of clopidogrel have _________